Olawuni, I. J. and Obuotor, E. M. and Obafemi, C. A. and Taiwo, F. O. (2021) Synthesis of Sulfanoquinoxaline-2,3-Dione Hydrazones Derivatives as a Selective Inhibitor for Acetylcholinesterase and Butyryl Cholinesterase. Journal of Applied Life Sciences International, 24 (8). pp. 8-16. ISSN 2394-1103
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Abstract
Some Sulfanoquinoxaline-2,3-diones hydrazone derivatives (1-8) were synthesized from the reactions of 2,3-dioxoquinoxaline-6-sulfonohydrazine with seven substituted benzaldehydes and acetophenone. All the synthesized compounds were biologically evaluated against cholinesterase’s (acetylcholinesterase and butyryl cholinesterase). Compounds 1-8 were found to be a good selective inhibitor for acetylcholinesterase and butyryl cholinesterase. Among the series, compounds 3 (IC50 = 75 ± 10 µg/mL) and 5 (IC50 = 80 ± 10 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 6 (IC50 = 110 ± 10 µg/mL), 8 (IC50 = 130 ± 10 µg/mL) and 7 (IC50 = 150 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase. The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50 = 70 ± 20 µg/mL). Their considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities make them a good candidate for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.
Item Type: | Article |
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Subjects: | Eurolib Press > Biological Science |
Depositing User: | Managing Editor |
Date Deposited: | 28 Jan 2023 06:30 |
Last Modified: | 13 Feb 2024 03:55 |
URI: | http://info.submit4journal.com/id/eprint/170 |